Assay Detail
Binding
CHEMBL4235697
Review assay metadata, readout intent, target linkage, and publication context from the same page.
Inhibition of BTK in human Ramos cells assessed as reduction in intracellular calcium level incubated for 1 hr measured for 180 secs by FLIPR assay
34
Total Activities
34
Compounds Tested
1
Activity Types
0
Assay Parameters
Assay Information
| Assay Type | Binding |
| Organism | Homo sapiens |
| Cell Type | Ramos |
| Confidence | 9 — Direct single protein target |
| Curated By | Autocuration |
Publication
Conversion of carbazole carboxamide based reversible inhibitors of Bruton's tyrosine kinase (BTK) into potent, selective irreversible inhibitors in the carbazole, tetrahydrocarbazole, and a new 2,3-dimethylindole series.
Activity Statistics
| Type | Count | Avg pChEMBL | Best pChEMBL |
|---|---|---|---|
| IC50 | 34 | 7.27 | 8.34 |
Compounds Tested
| Compound | Name | Phase | Activities | Best pChEMBL |
|---|---|---|---|---|
| CHEMBL4241958 | — | — | 1 | 8.34 |
| CHEMBL4248719 | — | — | 1 | 8.29 |
| CHEMBL4242527 | — | — | 1 | 8.19 |
| CHEMBL4239747 | — | — | 1 | 8.15 |
| CHEMBL4248550 | — | — | 1 | 8.06 |
| CHEMBL4237557 | — | — | 1 | 8.04 |
| CHEMBL4239031 | — | — | 1 | 7.82 |
| CHEMBL4245037 | — | — | 1 | 7.82 |
| CHEMBL4243995 | — | — | 1 | 7.80 |
| CHEMBL4248386 | — | — | 1 | 7.64 |
| CHEMBL4248271 | — | — | 1 | 7.64 |
| CHEMBL3918580 | — | — | 1 | 7.58 |
| CHEMBL4246324 | — | — | 1 | 7.58 |
| CHEMBL4237249 | — | — | 1 | 7.55 |
| CHEMBL4238798 | — | — | 1 | 7.47 |
| CHEMBL4248834 | — | — | 1 | 7.24 |
| CHEMBL4238256 | — | — | 1 | 7.23 |
| CHEMBL4242058 | — | — | 1 | 7.21 |
| CHEMBL4237999 | — | — | 1 | 7.20 |
| CHEMBL4246005 | — | — | 1 | 7.17 |
| CHEMBL4251151 | — | — | 1 | 7.12 |
| CHEMBL4237800 | — | — | 1 | 6.92 |
| CHEMBL4247992 | — | — | 1 | 6.77 |
| CHEMBL4249247 | — | — | 1 | 6.70 |
| CHEMBL4244928 | — | — | 1 | 6.54 |
| CHEMBL4240731 | — | — | 1 | 6.43 |
| CHEMBL4241723 | — | — | 1 | 6.05 |
| CHEMBL4238297 | — | — | 1 | 6.00 |
| CHEMBL4243299 | — | — | 1 | 5.77 |
| CHEMBL4238212 | — | — | 1 | 5.70 |
Activity Data
| Compound | Name | Type | Rel. | Value | Units | pChEMBL |
|---|---|---|---|---|---|---|
| CHEMBL4241958 | — | IC50 | = | 4.6 | nM | 8.34 |
| CHEMBL4248719 | — | IC50 | = | 5.1 | nM | 8.29 |
| CHEMBL4242527 | — | IC50 | = | 6.4 | nM | 8.19 |
| CHEMBL4239747 | — | IC50 | = | 7.1 | nM | 8.15 |
| CHEMBL4248550 | — | IC50 | = | 8.8 | nM | 8.06 |
| CHEMBL4237557 | — | IC50 | = | 9.2 | nM | 8.04 |
| CHEMBL4239031 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4245037 | — | IC50 | = | 15.0 | nM | 7.82 |
| CHEMBL4243995 | — | IC50 | = | 16.0 | nM | 7.80 |
| CHEMBL4248386 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL4248271 | — | IC50 | = | 23.0 | nM | 7.64 |
| CHEMBL3918580 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4246324 | — | IC50 | = | 26.0 | nM | 7.58 |
| CHEMBL4237249 | — | IC50 | = | 28.0 | nM | 7.55 |
| CHEMBL4238798 | — | IC50 | = | 34.0 | nM | 7.47 |
| CHEMBL4248834 | — | IC50 | = | 57.0 | nM | 7.24 |
| CHEMBL4238256 | — | IC50 | = | 59.0 | nM | 7.23 |
| CHEMBL4242058 | — | IC50 | = | 61.0 | nM | 7.21 |
| CHEMBL4237999 | — | IC50 | = | 63.0 | nM | 7.20 |
| CHEMBL4246005 | — | IC50 | = | 68.0 | nM | 7.17 |
| CHEMBL4251151 | — | IC50 | = | 75.0 | nM | 7.12 |
| CHEMBL4237800 | — | IC50 | = | 120.0 | nM | 6.92 |
| CHEMBL4247992 | — | IC50 | = | 170.0 | nM | 6.77 |
| CHEMBL4249247 | — | IC50 | = | 200.0 | nM | 6.70 |
| CHEMBL4244928 | — | IC50 | = | 290.0 | nM | 6.54 |
| CHEMBL4240731 | — | IC50 | = | 370.0 | nM | 6.43 |
| CHEMBL4241723 | — | IC50 | = | 890.0 | nM | 6.05 |
| CHEMBL4238297 | — | IC50 | = | 1000.0 | nM | 6.00 |
| CHEMBL4243299 | — | IC50 | = | 1700.0 | nM | 5.77 |
| CHEMBL4238212 | — | IC50 | = | 2000.0 | nM | 5.70 |
| CHEMBL4240879 | — | IC50 | - | — | - | |
| CHEMBL4245876 | — | IC50 | - | — | - | |
| CHEMBL4237436 | — | IC50 | > | 2000.0 | nM | - |
| CHEMBL4249677 | — | IC50 | > | 2000.0 | nM | - |